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抑制剂选择性比较

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所有产品 Rho抑制剂(25) 新Rho产品

产品目录	产品描述	文献引用	实验数据
S1314	Zoledronic Acid Zoledronic acid, 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。	Transl Oncol, 2018, 11(6):1406-1418 Oncoimmunology, 2017, 7(3):e1408745 Int J Cancer, 2016, 138(5):1281-9	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
S8031	NSC 23766 NSC 23766是一种Rac GTPase抑制剂，通过鸟嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化，无细胞试验中IC50为~50 μM；但是不会抑制密切相关的靶点，Cdc42或RhoA。	Neuron, 2019, 101(5):920-937 Proc Natl Acad Sci U S A, 2019, 116(8):2967-2976 Cell Rep, 2019, 27(12):3422-3432	MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
S7319	EHop-016 EHop-016 是一种特异性Rac GTPase抑制剂，在MDA-MB-435 和 MDA-MB-231细胞中作用于Rac1，IC50为1.1 μM，同等有效抑制Rac3。	Cancer Cell, 2019, 36(1):68-83 Cell Rep, 2019, 27(2):631-647 Mol Oncol, 2019, 10.1002/1878-0261.12548	(f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis.
S1721	Azathioprine Azathioprine 是一种抑制免疫系统的药物，抑制了嘌呤的合成以及GTP结合蛋白Rac1的激活，用于器官移植和自身免疫性疾病。	Sci Rep, 2019, 9(1):4360
S7293	ZCL278 ZCL278是一个选择性的Cdc42 GTP酶抑制剂，Kd为11.4 μM。	J Cell Physiol, 2018, 10.1002/jcp.27510 J Bone Miner Res, 2018, 33(5):945-958 J Virol, 2017, 91(5)	Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group.
S6752^New	Y16 Y16是G蛋白偶联Rho GEFs抑制剂。它能阻止LARG和Rho的结合，Kd值为80 nM。
S6527^New	Kobe2602 Kobe2602是选择性Ras抑制剂，抑制H-Ras GTP与c-Raf-1结合，Ki值为149 μM。
S8826^New	BAY-293 BAY-293可选择性抑制KRAS-SOS1相互作用，IC50为21 nM。
S8830^New	AMG510 AMG-510是有效的KRAS G12C共价抑制剂，具有潜在的抗肿瘤活性。
S7332	K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 是致癌的K-Ras(G12C)的变构抑制剂。
S7684	Salirasib Salirasib是一种有效的竞争性_{prenylated protein methyltransferase (PPMTase)}抑制剂， K_i为2.6 μM，其抑制_Ras甲基化。Phase 2。	Food Chem Toxicol, 2018, 119:464-478 Oncotarget, 2017, 8(30):49824-49838
S8749	MBQ-167 MBQ-167是一种有效的Rac和Cdc42双重抑制剂，在转移性乳腺癌细胞中，IC50分别为103 nM和78 nM。
S7719	CCG-1423 CCG-1423是一种特定的 RhoA 通路抑制剂，能够抑制SRF介导的转录。	Cancer Cell, 2019, 36(1):68-83 Cell Death Dis, 2019, 10(12):899 Cell Rep, 2018, 23(13):3798-3812	Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
S8469	CCG-203971 CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂，对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。
S7330	6H05 6H05是一个致癌K-Ras(G12C)的选择性、变构抑制剂。
S7331	K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12是致癌K-Ras(G12C)的变构抑制剂。	Oncotarget, 2016, 7(9):10064-72	(A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
S8303	Kobe0065 Kobe0065是H-Ras-cRaf1相互作用的抑制剂，能有效抑制H-Ras·GTP与c-Raf-1 RBD的结合，Ki值为46±13 μM。
S7333	K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 是一种变构的，选择性的致瘤性K-Ras(G12C)抑制剂。
S7607	BQU57 BQU57，RBC8的衍生物，是一种相对于GTPases Ras 和 RhoA的选择性GTPase Ral 抑制剂。
S8707	ARS-1620 ARS-1620是一种有效的、具有口服活性的KRAS^G12C共价抑制剂，在体内可产生迅速而持续地结合（占用）靶点，诱导肿瘤消退。	Clin Cancer Res, 2019, 10.1158/1078-0432 Cell Rep, 2019, 29(1):118-134
S8499	KRpep-2d KRpep-2d是选择性的K-Ras(G12D)抑制性环肽，相较于WT K-Ras和K-Ras(G12C)，对K-Ras(G12D)选择性更高，IC50为1.6 nM。
S8156	ARS-853 (ARS853) ARS-853是一种具有选择性的KRAS(G12C)共价结合抑制剂，通过结合GDP-肿瘤蛋白并阻止其激活，抑制突变型KRAS所驱动的信号通路。
S7482	EHT 1864 2HCl EHT 1864 2HCl是一种强效的Rac family GTPase抑制剂，其对Rac1, Rac1b, Rac2 和 Rac3的K_d分别为40 nM, 50 nM, 60 nM 和 250 nM 。	Nat Commun, 2019, 10(1):3667 Proc Natl Acad Sci U S A, 2019, 116(8):2967-2976 Cancers (Basel), 2019, 11(3)	E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
S7686	ML141 ML141是Rho家族GTPase cdc42的一种有效的，选择性可逆非竞争性抑制剂，IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。	J Pathol, 2019, 10.1002/path.5334 Front Microbiol, 2019, 10:1345 Front Pharmacol, 2019, 10:370	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
S5244	Zoledronic acid monohydrate Zoledronic acid，一种含氮的二磷酸盐，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。

产品目录	产品描述	文献引用	实验数据
S1314	Zoledronic Acid Zoledronic acid, 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。	Transl Oncol,2018, 11(6):1406-1418 Oncoimmunology,2017, 7(3):e1408745 Int J Cancer,2016, 138(5):1281-9	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
S8031	NSC 23766 NSC 23766是一种Rac GTPase抑制剂，通过鸟嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化，无细胞试验中IC50为~50 μM；但是不会抑制密切相关的靶点，Cdc42或RhoA。	Neuron,2019, 101(5):920-937 Proc Natl Acad Sci U S A,2019, 116(8):2967-2976 Cell Rep,2019, 27(12):3422-3432	MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
S7319	EHop-016 EHop-016 是一种特异性Rac GTPase抑制剂，在MDA-MB-435 和 MDA-MB-231细胞中作用于Rac1，IC50为1.1 μM，同等有效抑制Rac3。	Cancer Cell,2019, 36(1):68-83 Cell Rep,2019, 27(2):631-647 Mol Oncol,2019, 10.1002/1878-0261.12548	(f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis.
S1721	Azathioprine Azathioprine 是一种抑制免疫系统的药物，抑制了嘌呤的合成以及GTP结合蛋白Rac1的激活，用于器官移植和自身免疫性疾病。	Sci Rep,2019, 9(1):4360
S7293	ZCL278 ZCL278是一个选择性的Cdc42 GTP酶抑制剂，Kd为11.4 μM。	J Cell Physiol,2018, 10.1002/jcp.27510 J Bone Miner Res,2018, 33(5):945-958 J Virol,2017, 91(5)	Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group.
S6752^New	Y16 Y16是G蛋白偶联Rho GEFs抑制剂。它能阻止LARG和Rho的结合，Kd值为80 nM。
S6527^New	Kobe2602 Kobe2602是选择性Ras抑制剂，抑制H-Ras GTP与c-Raf-1结合，Ki值为149 μM。
S8826^New	BAY-293 BAY-293可选择性抑制KRAS-SOS1相互作用，IC50为21 nM。
S8830^New	AMG510 AMG-510是有效的KRAS G12C共价抑制剂，具有潜在的抗肿瘤活性。
S7332	K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 是致癌的K-Ras(G12C)的变构抑制剂。
S7684	Salirasib Salirasib是一种有效的竞争性_{prenylated protein methyltransferase (PPMTase)}抑制剂， K_i为2.6 μM，其抑制_Ras甲基化。Phase 2。	Food Chem Toxicol,2018, 119:464-478 Oncotarget,2017, 8(30):49824-49838
S8749	MBQ-167 MBQ-167是一种有效的Rac和Cdc42双重抑制剂，在转移性乳腺癌细胞中，IC50分别为103 nM和78 nM。
S7719	CCG-1423 CCG-1423是一种特定的 RhoA 通路抑制剂，能够抑制SRF介导的转录。	Cancer Cell,2019, 36(1):68-83 Cell Death Dis,2019, 10(12):899 Cell Rep,2018, 23(13):3798-3812	Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
S8469	CCG-203971 CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂，对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。
S7330	6H05 6H05是一个致癌K-Ras(G12C)的选择性、变构抑制剂。
S7331	K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12是致癌K-Ras(G12C)的变构抑制剂。	Oncotarget,2016, 7(9):10064-72	(A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
S8303	Kobe0065 Kobe0065是H-Ras-cRaf1相互作用的抑制剂，能有效抑制H-Ras·GTP与c-Raf-1 RBD的结合，Ki值为46±13 μM。
S7333	K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 是一种变构的，选择性的致瘤性K-Ras(G12C)抑制剂。
S7607	BQU57 BQU57，RBC8的衍生物，是一种相对于GTPases Ras 和 RhoA的选择性GTPase Ral 抑制剂。
S8707	ARS-1620 ARS-1620是一种有效的、具有口服活性的KRAS^G12C共价抑制剂，在体内可产生迅速而持续地结合（占用）靶点，诱导肿瘤消退。	Clin Cancer Res,2019, 10.1158/1078-0432 Cell Rep,2019, 29(1):118-134
S8499	KRpep-2d KRpep-2d是选择性的K-Ras(G12D)抑制性环肽，相较于WT K-Ras和K-Ras(G12C)，对K-Ras(G12D)选择性更高，IC50为1.6 nM。
S8156	ARS-853 (ARS853) ARS-853是一种具有选择性的KRAS(G12C)共价结合抑制剂，通过结合GDP-肿瘤蛋白并阻止其激活，抑制突变型KRAS所驱动的信号通路。
S7482	EHT 1864 2HCl EHT 1864 2HCl是一种强效的Rac family GTPase抑制剂，其对Rac1, Rac1b, Rac2 和 Rac3的K_d分别为40 nM, 50 nM, 60 nM 和 250 nM 。	Nat Commun,2019, 10(1):3667 Proc Natl Acad Sci U S A,2019, 116(8):2967-2976 Cancers (Basel),2019, 11(3)	E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
S7686	ML141 ML141是Rho家族GTPase cdc42的一种有效的，选择性可逆非竞争性抑制剂，IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。	J Pathol,2019, 10.1002/path.5334 Front Microbiol,2019, 10:1345 Front Pharmacol,2019, 10:370	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
S5244	Zoledronic acid monohydrate Zoledronic acid，一种含氮的二磷酸盐，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。

研究领域

产品类型

Rho

信号通路图

研究领域

抑制剂选择性比较

Rho产品